首页> 外国专利> FLUORINATED QUINOLINE AND QUINOXALINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES

FLUORINATED QUINOLINE AND QUINOXALINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES

机译:氟化喹啉和喹喔啉衍生物作为二氢脱氢酶(Dhodh)抑制剂,用于治疗癌症,自身免疫和炎症性疾病

摘要

The present invention discloses compounds formula (I): (I) wherein X is CH; The present compounds of formula (I) are dihydroorotate dehydrogenase (DHODH) inhibitors, and are useful for the treatment of inflammatory disorders, autoimmune disorders and cancer, such as e.g. lymphomas, leukemias, carcinomas, and sarcomas. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 60 to 136; examples 1 to 39; tables 1 and 2). An exemplary compound is e.g. : 4-ethyl-1-(7-fluoro-4-isopropyl-2- (2-methoxyphenyl)quinolin-6-yl)-3-(hydroxymethyl)-1H-1,2,4- triazol-5(4H)-one (example 1): (AA)
机译:本发明公开了化合物式(I):(I),其中X是CH;本式(I)化合物是二羟色酸盐脱氢酶(DHODH)抑制剂,可用于治疗炎性疾病,自身免疫病症和癌症,例如例如,淋巴瘤,白血病,癌症和肉瘤。本说明书公开了示例性化合物的合成和表征及其药理学数据(例如,第60至136页;实施例1至39;表1和2)。示例性化合物是例如:4-乙基-1-(7-氟-4-异丙基-2-(2-甲氧基苯基)喹啉-6-基)-3-(羟甲基)-1H-1,2,4-三唑-5(4H) -one(例1):( AA)

著录项

  • 公开/公告号WO2021084500A1

    专利类型

  • 公开/公告日2021-05-06

    原文格式PDF

  • 申请/专利权人 JANSSEN BIOTECH INC.;

    申请/专利号WO2020IB60221

  • 发明设计人 CISAR JUSTIN;KEOHANE COLLEEN;KUDUK SCOTT;

    申请日2020-10-30

  • 分类号C07D401/04;C07D403/04;C07D401/14;A61K31/4709;A61K31/4196;A61K31/517;A61K31/4155;A61K31/444;A61K31/4439;A61K31/351;A61P29;A61P35;A61P35/02;A61P37;A61P37/02;A61P37/06;

  • 国家 IB

  • 入库时间 2022-08-24 18:36:54

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